Detail of "34184-77-5"

Reference

Binding of [3H]-methyltrienolone (R 1881) in rat prostate and human benign prostatic hypertrophy (BPH)

Binding of [3H]-methyltrienolone (R 1881) in rat prostate and human benign prostatic hypertrophy (BPH). Asselin, Jacques; Labrie, Fernand; Gourdeau, Yves; Bonne, Claude; Raynaud, Jean P.Several substances are used for example 57-83-0 and 797-63-7 which are their cas registry numbers. (Cent. Hosp., Univ. Laval, Quebec, Que., Can.). Steroids, 28(4), 449-59 (English) 1976. CODEN: STEDAM. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Section cross-reference(s): 14 Methyltrienolone (I) [965-93-5] binding to rat ventral prostate cytosol had a specificity typical of an androgen receptor. In human benign prostatic hypertrophy (BPH) tissue, the specificity of I-3H binding was different from that measured in rat prostate: progesterone [57-83-0] and R 5020 [34184-77-5] were more potent whereas 19-nortestosterone [434-22-0] was a less potent competitor. Moreover, the synthetic progestin R 5020-3H bound to BPH tissue with a similar specificity. These data suggest the presence of progestin binding components or of an atypical androgen receptor in human BPH cytosol. .

Characterization and assay of progesterone receptor in human mammary carcinoma

Characterization and assay of progesterone receptor in human mammary carcinoma. Pichon, M. F.; Milgrom, E. (Groupe Rech. Biochim. Endocr. Reprod., Fac. Med. Paris-Sud, Bicetre, Fr.). Cancer Res., 37(2), 464-71 (English) 1977. CODEN: CNREA8. DOCUMENT TYPE: Journal CA Section: 2 (Hormone Pharmacology) Section cross-reference(s): 9 Tritium-labeled progesterone (I) [57-83-0]-receptor complexes from human mammary carcinoma stabilized in the presence of glycerol. The dissocn. rate const. was lowered and the equil.There are some reagents with their cas registry numbers 128-23-4 and 566-65-4 are used in this study. dissocn. const. was decreased (KD = 3 nM in the absence of glycerol and 1.1 nM in the presence of 30% glycerol), whereas no clear-cut effect on the assocn. rate was obsd. and no change occurred in the concn. of binding sites. Cortisol [50-23-7] competed with I-3H only at concns. >1 .mu.M. Synthetic progestins chlormadinone acetate [302-22-7], norethisterone [68-22-4], and F5020 [34184-77-5] had a high affinity for the receptor whereas 5.alpha.-pregnane-3,20-dione [566-65-4] had an affinity .apprx.50% that of I itself. 5.beta.-Pregnane-3,20-dione [128-23-4], 17.alpha.-hydroxypregn-4-ene-3,20-dione [68-96-2], corticosterone [50-22-6], estradiol [50-28-2], and testosterone [58-22-0] were weak inhbitors of I-3H binding. I-3H specific binding having the characteristics of receptor was found either in the 8 S region , in the 4.5 S region, or in both. Activated I receptor complex was bound to human DNA. An assay of the receptor based on these binding properties is described. This assay measures the total concn. of cytosol receptor since it makes possible the exchange of endogenous hormone for excess added [3H]progesterone. Of 55 biopsies examd. by this method, 65 had a concn. of I receptor-binding sites >10 fmol/mg protein. There was a pos. correlation between the amts. of estrogen and I receptors. .